-Escin: An Updated Review of Its Analysis, Pharmacology, Pharmacokinetics, and Toxicity

beta-Escin is an oleanane-type pentacyclic triterpenoid saponin extracted from the seeds of Aesculus hippocastanum (AH), which is more widely distributed. beta-Escin sodium has been approved by the American FDA for clinical usage. This paper is intended to summarize an updated and comprehensive review of the pharmacological activities, pharmacokinetic properties, toxicity, and analytical methods of beta-escin. Studies have shown that beta-escin has significant antitumor, antiviral, anti-inflammatory, and other activities alongside less adverse effects and higher safety than other compounds. The review shows that the pharmacological effects of beta-escin involve mechanisms such as ATM/gamma H2AX, RhoA/Rock, GSK-3 beta/beta-Catenin, HER2/HER3/Akt, and PI3K/Akt signaling pathways, and Cyclin A, p21(WAF1/CIP1), survivin, Bcl-2, Mcl-1, Caspases, TGF-beta, MMPs, and TNF-alpha, among other inflammatory factors. beta-Escin has significant cytotoxicity; the use of the chitosan/xanthan gum-based polyelectrolyte complexes PA1 and PC-11 to modify it not only to reduces its toxicity, but also improves its drug efficacy. Because of this, these compounds may become a new research hotspot. beta-Escin in vivo metabolism can be converted by the CYP1A2 enzyme in the intestinal flora to produce alpha-escin, deacylated, deglycosylated, and 21 beta-O-crotonoyl-protoescin, and the binding rate of the plasma proteins is higher than 90%. These are mainly metabolized by the liver, kidneys, and other organs, and excreted in the form of urine and feces. The number of reports on the specific mediators of the metabolism of beta-escin and their mechanisms and metabolites is relatively small; furthermore, the results are vague. Therefore, a complete and in-depth exploration of the pharmacokinetic characteristics of beta-escin is needed to provide a more complete and effective theoretical reference for the study of its pharmacodynamic activity.